Ion channel drugs on the market – Ion channel library

Name	Brand names	Mechanism of action	Indication	Type	Year of Approval	Company
Amlodipine	Norvasc, Aforbes	Cav1.x inhibitor	Hypertension, vasospastic angina, angina pectoris	Small molecule	1992	Pfizer
Ajmaline		Nav1.5 inhibitor	Arrhythmia	Small Molecule
Alosetron	Lotronex	5HT3A antagonist	Irritable bowel syndrome with diarrhea	Small molecule	2002 FDA
Alprazolam	Xanax	GABA-A positive modulator	Anxiety	Small molecule	1981 FDA	Upjohn
Amantadine	Symadine, Osmolex	GluN inhibitor	Parkinson's disease	Small molecule
Amifampridine	Firdapse	Kv blocker	Lambert-Eaton myasthenic syndrome	Small molecule	2009	BioMarin
Amiloride	Midamor	ENaC inhibitor	Hypertensive disorder, edema, hypokalemia	Small molecule	1981
Amiodarone	Cordarone	Kv11.1 blocker	Ventricular fibrillation, life-threatening ventricular tachycardia	Small molecule	1961
Atracurium		Chrn abd antagonist	General anaesthesia, muscle relaxation	Small Molecule	1983 FDA
Azelnidipine	CalBlock	Cav1.x blocker	Hypertension	Small Molecule		Daiichi-Sankyo
Benzocaine	Anacaine, Dermoplast	Nav blocker	Local anesthesia	Small Molecule
Bioallethrin		Sodium channel (Pediculus humanus) modulator	Lice and scabies infestation	Small Molecule
Brexanolone	Zulresso	GABA-A positive modulator	Postpartum depression	Small Molecule	2019	Sage Therapeutics
Bupivacaine	Marcaine	Nav inhibitor	Local anesthesia	Small molecule	1972 FDA	Hospira
Butalbital	Sandoptal	GABA-A potentiator	Tension-type headache	Small Molecule	1976	Actavis Labs
Capsaicin	Zostrix, Qutenza	TRPV1 activator	Neuralgia, postherpetic neuralgia, backache, arthritic pain	Small molecule	2009 FDA	Acorda Therapeutics
Carbamazepine	Actebral, Tegretol	Nav1.5 blocker	Epilepsy, Lennox-Gastaut syndrome, bipolar disorder	Small molecule	1968	Novartis
Carbutamide	Glucidoral	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1956	Servier
Chlordiazepoxide	Risolid	GABAA positive modulator	Anxiety, alcohol withdrawal syndrome	Small molecule	1960 FDA	Valeant
Chloroprocaine	Nesacaine	Nav1.8 inhibitor	Local anesthesia	Small Molecule
Chlorpropamide		Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1958	Pfizer
Chlorzoxazone	Parafon, Paraflex	KCa activator	Spasticity, muscle spasm with pain	Small molecule	1958	Janssen
Cilnidipine	Atelec, Cilogard	Cav1.x blocker, Cav2.2 blocker	Hypertension	Small Molecule	1995	Fuji Viscera, Ajinomoto
Cinchocaine	Dibucaine, Nupercainal	Nav blocker	Local anesthesia	Small Molecule
Cinnarizine	Stugeron, Cinazyn	Cav inhibitor	Vertigo, motion sickness, nausea	Small molecule	1955	Jansen Pharmaceutica
Cisatracurium	Nimbex	Chrn a1b1d inhibitor	General anaesthesia, muscle relaxation	Small molecule	1995 FDA
Clevidipine	Cleviprex	Cav1.x blocker	Hypertension	Small molecule	2008	The Medicines Company
Clobazam	Frisium, Urbanol, Onfi, Tapclob	GABAA partial agonist	Epilepsy, anxiety	Small molecule	2011	Lundbeck
Clonazepam	Clonapam, Rivotril	GABAA positive modulator	Myoclonic, atonic and absence seizures; Lennox-Gastaut syndrome	Small molecule	1975	Roche
Clorazepate	Tranxene	GABAA positive modulator	Anxiety, alcohol withdrawal syndrome, partial epilepsy	Small molecule	1972
Clotiazepam	Clozan	GABA-A potentiator	Anxiety disorders	Small Molecule
Crofelemer	Mytesi, Fulyzaq	CFTR inhibitor, ANO1 inhibitor	Non-infectious diarrhea	Small Molecule	2012	Salix Pharmaceuticals
Cyclandelate	Cyclospasmol	Cav alpha-2/delta-1 modulator	Arteriosclerosis, Raynaud's disease	Small Molecule
Dalfampridine	Ampyra, Fampyra	Kv blocker	Multiple sclerosis	Small molecule	2010	Acorda Therapeutics
Dantrolene	Dantrium	RyR1 inhibitor	Spasticity, malignant hyperthermia	Small molecule	1974	Par Pharmaceutical
Desflurane	Suprane	GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anestesia	Small Molecule	1992	Baxter
Dextromethorphan		GluN3A antagonist	Cough, rhinitis, sneezing	Small Molecule	1957	ANI Pharmaceuticals
Diazepam	Valium, Diastat	GABA-A potentiator	Anxiety, alcohol withdrawal syndrome, spasticity, epilepsy	Small molecule	1963 FDA	Roche
Diazoxide	Proglycem	Kir6.2 activator	Hypertensive emergencies, hyperinsulinism	Small molecule	1973
Diltiazem	Cardizem, Tiazac	Cav1.x inhibitor	Hypertension, angina pectoris	Small molecule	1982
Disopyramide	Norpace, Ritmodan, Dicorantil	Nav1.5 inhibitor	Ventricular arrhythmia	Small molecule	1977	G.D. Searle LLC
Dofetilide	Tikosyn	Kir2.2, Kv10.1, Kv11.1 inhibitor	Atrial fibrillation, atrial flutter	Small molecule	1999	Pfizer
Dronedarone	Multaq	Multichannel blocker	Atrial fibrillation	Small molecule	2009 FDA	Sanofi-Aventis
Efonidipine	Landel	Cav1.x inhibitor, Cav3.x inhibitor	Hypertension	Small molecule	1995
Enflurane	Ethrane, Alyrane	GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anestesia	Small Molecule	1972	Baxter
Eslicarbazepine	Aptiom, Zebinix, Exalief	Nav inhibitor	Partial seizures	Small molecule	2009 EMA 2013 FDA	Bial
Estazolam	Prosom, Eurodin, Nuctalon	GABAA potentiator	Severe Insomnia	Small molecule	1990	Abbott
Eszopiclone	Lunesta	GABA-A potentiator	Insomnia	Small molecule	2004	Sunovion
Ethosuximide	Zarontin	Cav3.1 inhibitor	Absence seizures	Small molecule	1960	Parke Davis
Etidocaine	Duranest	Nav inhibitor	Local anesthesia	Small molecule	1976 FDA
Felbamate	Felbatol	GluN antagonist	Epilepsy, Lennox-Gastaut syndrome	Small molecule	1993 FDA
Felodipine	Plendil	Cav1.x blocker, Cav3.x blocker	Hypertension, Angina pectoris prophylaxis	Small molecule	1991	AstraZeneca
Flecainide	Tambocor	Nav1.4 and Nav1.5 blocker	Atrial fibrillation, atrial flutter, life-threatening ventricular tachycardia	Small molecule	1985
Flumazenil	Anexate, Romazicon	GABA-A antagonist	Benzodiazepine induced sedation or toxicity	Small molecule	1991 FDA	Hoffman La Roche
Flunarizine	Sibelium	Cav3.x inhibitor	Migraine, epilepsy, vertigo	Small molecule	1968	Jansen Pharmaceutica
Flunitrazepam	Hypnodorm	GABA-A potentiator	Severe insomnia, anxiety	Small Molecule	1976
Flupirtine	Katadolon	Kv7.2-Kv7.5 activator	Acute and chronic pain	Small molecule	1984	Asta-Medica
Flurazepam	Dalmadorm, Dalmane	GABAA activator	Insomnia	Small molecule	1970
Fluspirilene	Redeptin, Imap	Cav inhibitor	Schizophrenia	Small molecule	1963	Jansen Pharmaceutica
Fosphenytoin	Cerebyx	Nav1.5 blocker	Epilepsy	Small molecule	1996	Parke-Davis
Funapide	TV-45070, XEN402	Nav1.7 and Nav1.8 blocker	Chronic pain	Small Molecule		Xenon Pharmaceuticals
Gabapentin	Neurontin	Cav alpha-2/delta inhibitor, GluN inhibitor	Postherpetic neuralgia, partial seizures	Small molecule	1993	Pfizer
Glibenclamide	Diabeta, Glyburide	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1984	Sanofi Aventis
Glibornuride	Glutril	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1969/
Gliclazide	Diamicron	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1972
Glimepiride	Amaryl	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1995	Sanofi Aventis
Glipizide	Glucotrol	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1984	Pfizer
Gliquidone	Glurenorm	Kir6.2 blocker	Diabetes mellitus type 2	Small Molecule
Glisoxepide		Kir6.x inhibitor	Diabetes mellitus type 2	Small molecule
Glyclopyramide	Deamelin	Kir6.x inhibitor	Diabetes mellitus type 2	Small molecule	1965
Glymidine	Glycanol	Kir inhibitor	Diabetes mellitus type 2	Small Molecule
Granisetron	Kytril	5HT3A antagonist	Therapy-induced nausea and vomiting	Small molecule	1993 FDA
Halothane		GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anesthesia	Small Molecule	1958 FDA
Hexylcaine	Cyclaine	Nav blocker	Local anesthesia	Small Molecule		Merck
Ibutilide	Corvert	Kv11.1 blocker	Atrial fibrillation, atrial flutter	Small Molecule	1995
Isoflurane	Isorane, Aerrane	GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist	General anestesia	Small Molecule	1979	Baxter
Isradipine	DynaCirc, Prescal, Clivoten, Esradin, Lomir	Cav1.x blocker	Hypertension	Small molecule	1989	Sandoz (now division of Novartis)
Ivabradine	Corlanor, Corlentor	HCN inhibitor	Chronic heart failure, angina pectoris	Small molecule	2005 EMA 2015 FDA	Servier, Amgen
Ivacaftor	Kalydeco	CFTR potentiator	Cystic fibrosis	Small molecule	2012	Vertex Pharmaceuticals
Ketamine	Ketalar	GluN antagonist	General and local anaesthesia	Small molecule	1970 FDA
Ketazolam	Loftran, Anseren	GABA-A potentiator	Anxiety	Small Molecule
Lacidipine	Lacipil, Motens	Cav1.x blocker	Hypertension	Small Molecule
Lacosamide	Vimpat	Nav inhibitor	Partial epilepsy	Small molecule	2008 FDA 2008 EMA	UCB
Lamotrigine	Lamictal	Nav inhibitor	Tonic-clonic seizures, epilepsy, Lennox-Gastaut syndrome	Small molecule	1994	GSK
Leconotide		Cav2.2 blocker	Pain	Peptide
Lercanidipine	Zanidip	Cav1.x inhibitor	Hypertension	Small molecule	1997
Levamlodipine	Asomex, Espin	Cav1.x blocker	Hypertension, angina	Small Molecule
Levobupivacaine	Chirocaine	Nav inhibitor	Local anesthesia	Small molecule	1999 FDA	Purdue pharma
Levomenthol	Menthol	TRPM8 agonist	Minor irritation, pain, sore mouth, sore throat, itching, local anesthesia	Small Molecule
Lidocaine	Xylocaine	Nav blocker	Local anaesthesia, neuralgia, itching, pediculosis, ventricular arrhythmia	Small molecule	1948	Fresenius Kabi
Lorazepam	Ativan	GABAA activator	Anxiety, Myoclonic seizure, Atonic seizure, Status epilepticus	Small molecule	1977 FDA	Wyeth Pharmaceuticals
Lormetazepam		GABA-A potentiator	Short-term insomnia	Small Molecule
Lubiprostone	Amitiza	CLC-2 activator	Chronic idiopathic constipation	Small Molecule	2006	Sucampo Pharmaceuticals
Lumacaftor	Orkambi (a combination of ivacaftor and lumacaftor)	CFTR modulator	Cystic fibrosis	Small molecule	2015	Vertex Pharmaceuticals
Manidipine	Calslot, Manyper	Cav1.x and Cav3.x blocker	Hypertension	Small Molecule
Mavatrep		TRPV1 antagonist	Pain	Small Molecule		Janssen
Memantine	Axura, Namenda	GluN antagonist	Moderate to severe Alzheimer's type dementia	Small molecule	2003	Forest labs
Mepivacaine	Carbocaine	Nav inhibitor	Local anesthesia	Small molecule	1960 FDA	Hospira, Inc., Pfizer
Methoxyflurane	Penthrox	GABA-A activator, GluA1 inhibitor, GLYRA1 agonist	General anestesia	Small Molecule		Abbott
Methsuximide	Petinutin	Cav3.x blocker	Absence seizures, epilepsy	Small Molecule	1957	Parke Davis
Mexiletine	Mexitil	Nav inhibitor	Ventricular arrhythmia	Small molecule	1985
Midazolam	Buccolam, Versed	GABA-A activator	Anxiety, Anesthesia, Status epilepticus	Small molecule	1985
Minoxidil	Loniten	Kir6.2 activator	Hypertension, alopecia	Small molecule	1979 FDA
Mirogabalin	Tarlige	Cav ?2? modulator	Peripheral neuropathic pain			Daiichi Sankyo
Nateglinide	Starlix	Kir6.2 blocker	Diabetes mellitus type 2	Small molecule	2000 FDA	Novartis
Nicardipine	Cardene	Cav1.x inhibitor	Hypertension, angina pectoris	Small molecule	1988
Nicorandil	Ikorel, Dancor	Kir6.2 activator	Angina pectoris	Small molecule	1984
Nicotine	Nicorette, Nicotrol	Chrn agonist	Smoking cessation, nicotine dependence	Small molecule
Nifedipine	Adalat, Procardia, Afeditab, Nifediac	Cav1.x blocker	Hypertension, vasospastic angina, premature labor	Small molecule	1981	Pfizer
Nilvadipine	Escor, Escor forte, Naftdil, Nilvadipine, Nivadil, Towajil	calcium channel blocker	hypertension, vasospastic angina, chronic stable angina	Small Molecule		Astellas Pharma, Archer Pharmaceuticals
Nimodipine	Nimotop, Nymalize	Cav1.x blocker	Subarachnoid hemorrhage, hypertension	Small molecule	1988
Nisoldipine	Sular	Cav1.x blocker	Hypertension	Small Molecule	1995	Shionogi
Nitrazepam	Mogadon, Alodorm, Nitrazadon	GABA-A potentiator	Insomnia	Small molecule	1965
Nitrendipine	Baypress, Nidrel	Cav1.x blocker	Hypertension	Small Molecule	1985
Ondansetron	Zophren	5HT3A antagonist	Therapy-induced nausea and vomiting	Small molecule	1991 FDA	GSK
Oxazepam	Novoxapam, Alepam	GABA-A potentiator	Anxiety, alcohol withdrawal delirium	Small molecule	1965
Oxcarbazepine	Trileptal	Nav1.5 blocker	Epilepsy	Small molecule	1990
Oxybuprocaine	Novesine, Novesin	Nav inhibitor	Local anesthesia	Small Molecule
Palonosetron	Aloxi	5HT3A antagonist	Chemotherapy-induced nausea and vomiting	Small molecule	2003 FDA 2009 EMA	Helsinn Healthcare
Pentolinium		NACHR antagonist	Hypertension	Small Molecule		Wyeth Pharmaceuticals
Perampanel	Fycompa	GluA1-4 antagonist	Partial seizures	Small molecule	2012 FDA	Eisai
Permethrin	Elimite	Sodium channel (Sarcoptes scabiei) inhibitor	Infestation by Sarcoptes scabiei, Pediculosis	Small Molecule	1986
Phenobarbital	Luminal	GABA-A potentiator	Epilepsy, Lennox-Gastaut syndrome, migraine	Small molecule	1912
Phensuximide	Milontin	Cav inhibitor Nav inhibitor	Epilepsy, absence seizures	Small molecule	FDA	Parke Davis
Phenytoin	Dilantin	Nav inhibitor	Epilepsy	Small molecule	1953	Parke Davis
Pinacidil	Pindac	Kir6.2 activator	Hypertension	Small molecule	1989 FDA	Leo Pharma
Pinaverium	Dicetel	Cav1.x antagonist	Irritable bowel syndrome	Small molecule	1975	Solvay Pharmaceuticals
Pregabalin	Lyrica	Cav alpha-2/delta modulator	Diabetic peripheral neuropathy, postherpetic neuralgia	Small molecule	2004
Prilocaine	Citanest, Xylonest	Nav inhibitor	Local anaesthesia, premature ejaculation	Small molecule	1965
Primidone	Mysoline	GABA-A positive modulator	Epilepsy, Lennox-Gastaut syndrome	Small molecule	1954 FDA	Valeant
Procainamide	Pronestyl, Procan-SR, Procanbid	Nav inhibitor, Kv11.1 inhibitor	Life-threatening ventricular tachycardia	Small molecule	1950	Bristol-Meyers Squibb
Procaine	Novocaine	Nav1.8 blocker	Local anesthesia	Small Molecule	1954
Propafenone	Rythmol	Nav1.5 blocker	Atrial fibrillation, atrial flutter, life-threatening ventricular tachycardia	Small molecule	1989	GSK
Proparacaine	Alcaine, Ophthetic	Nav blocker	Local anesthesia	Small Molecule	1953
Propofol	Diprivan	GABA-A potentiator	General anaesthesia	Small molecule	1989 FDA	Fresenius Kabi
Quazepam	Doral, Dormalin	GABA-A potentiator	Insomnia	Small molecule	1985	Sciencure Pharma
Quinidine	Cardioquin, Quinidex	Nav inhibitor	Atrial fibrillation, malaria, life-threatening ventricular tachycardia	Small Molecule	1950	Lilly
Ranolazine	Ranexa	Nav inhibitor	Angina pectoris	Small molecule	2006	Gilead
Repaglinide	Gluconorm, Prandin, Novonorm	Kir6.2 blocker	Diabetes mellitus type 2	Small molecule	1997	Novo Nordisk
Riluzole	Rilutek	KCa2.3 activator, Nav1.5 inhibitor	Amyotrophic lateral sclerosis	Small molecule	1995 FDA
Rocuronium	Zemuron, Esmeron	Chrn a1b1d/g antagonist	General anaesthesia, muscle relaxation	Small molecule	1994 FDA
Ropivacaine	Naropin	Nav blocker	Local anaesthesia	Small molecule	1996	Fresenius Kabi
Rufinamide	Banzel	Nav modulator	Lennox-Gastaut syndrome	Small Molecule	2007 EMA 2008 FDA	Novartis
Safinamide	Xadago	Nav and Cav inhibitor	Parkinsons disease	Small Molecule	2015 EMA 2017 FDA	Newron Pharmaceuticals
Sevoflurane	Ultane, Sojourn	GABA-A activator, GLYRA1 agonist	General anestesia	Small Molecule	1995	Abbvie
Sotalol	Biosotal, Sotalex	Kv11.1 blocker	Atrial fibrillation, life-threatening ventricular tachycardia	Small molecule	1974
Stiripentol	Diacomit	GABA-A positive modulator	Myoclonic seizures	Small Molecule	2007 EMA 2018 FDA	Biocodex
Succinylcholine	Anectine	Chrn a1b1deg agonist	General anaesthesia, muscle relaxation	Small molecule	1952 FDA	Sandoz
Temazepam	Restoril	GABA-A potentiator	Insomnia	Small molecule	1981	Mallinckrodt Pharmaceuticals
Tetracaine	Pontocaine	Nav inhibitor	Local anesthesia	Small molecule	1941
Tezacaftor		CFTR activator	Cystic fibrosis	Small Molecule	2018	Vertex Pharmaceuticals
Tocainide	Tonocard	Nav blocker	Ventricular arrhythmia	Small Molecule	1984
Tolazamide	Tolinase, Norglycin	Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1966
Tolbutamide		Kir6.2 inhibitor	Diabetes mellitus type 2	Small molecule	1961 FDA
Topiramate	Topamax	GABA-A positive modulator, Nav blocker, GluA antagonist	Epilepsy, migraine, Lennox-Gastaut syndrome	Small Molecule
Triamterene	Dyrenium	ENaC inhibitor	Hypertensive disorder, edema	Small molecule	1964	Smith Kline & French
Triazolam	Halcion	GABA-A positive modulator	Insomnia	Small molecule	1982 (withdrawn in the UK)	Pharmacia and Upjohn
Trimebutine	Trimebutine	Cav1.x inhibitor, KCa inhibitor	Irritable bowel syndrome, postoperative paralytic ileus	Small Molecule
Trimethadione	Tridione	Cav3.1 inhibitor	Absence seizures, epilepsy	Small Molecule	1946	Abbvie
Unoprostone	Rescula	BK and CLC-2 activator	Ocular hypertension, open-angle glaucoma	Small Molecule	2000 FDA (discontinued in the US)	Sucampo Pharmaceuticals
Valproic acid	Convulex, Depakene, Valcote	Nav inhibitor, GABAA modulator	Epilepsy, absence seizures, bipolar disorder, migraine	Small molecule
Varenicline	Chantix, Champix	Chrn a4b2 agonist	Smoking cessation	Small molecule	2006 FDA	Pfizer
Verapamil	Calan, Verelan	Cav1.x inhibitor	Hypertension, angina, supraventricular tachycardia, migraine, cluster headache	Small molecule	1981
Vernakalant	Brinavess	Nav1.5, Kv1.5, Kv4.3 blocker	Atrial fibrillation	Small Molecule	2010, EMA	Cardiome Pharma
XEP-018		NaV1.4 blocker	Skin wrinkles	Synthetic peptide		Activen
Zaleplon	Sonata	GABA-A agonist	Insomnia	Small Molecule	1999	Meda Ab, Pfizer
Ziconotide	Prialt	Cav2.2 blocker	Severe and chronic pain	Synthetic peptide	2004	Elan Pharmaceuticals
Zolpidem	Ambien	GABA-A agonist	Insomnia	Small molecule	1992	Sanofi Aventis
Zonisamide	Zonegran	Nav blocker, Cav3.x blocker	Partial epilepsy	Small Molecule	2000	Eisai
Zopiclone	Imovane, Zimovane	GABA-A potentiator	Insomnia	Small molecule	1986	Rhône-Poulenc
Zucapsaicin	Zuacta	TRPV1 agonist	Severe pain associated with osteoarthritis of the knee, neuropathic pain	Small Molecule		Sanofi Aventis